Tumor diagnosis at early stage before its metastasis is critical to improve the survival of patients. We have developed a novel Multifunctional Agent for image-guided (PET/fluorescence) surgery with an option of Photodynamic therapy (PDT). in a recent study with a corresponding radioactive (I124-) analog, we were able to detect the primary and distant lesions from a breast tumor model known to metastasize to lung and bones. These results are exciting and provide an opportunity to use the PS (in combination with radioactive & nonradioactive analog) to image lung tumors by PET, and then treat them either by fluorescence-guided surgery in combination with PDT and/or chemotherapy. In a parallel study, we have shown that cell specificity of the iodinated PS in 3D culture system derived from cancer patients and the photo-induced STAT-3 dimerization can be used as a biomarker in optimizing the PDT treatment parameters in patients. We extrapolate that translating these findings to clinic will markedly change the treatment paradigm for loco-regional non-small cell lung cancer and will result in improved outcomes. Detection of occult lymph node disease will be enhanced and intraoperative adjuvant photodynamic therapy can be accomplished. Additionally, patients whose comorbidities preclude surgical resection can have a repeatable, effective PDT.